Modulation of the activity of human plasma esterases by binary and ternary mixtures of water miscible organic solvents during in vitro drug metabolism studies
By: Nesarikar, Mugdha
.
Contributor(s): Gupta, V.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2023Edition: Vol.85(4), Jul-Aug.Description: 1157-1162p.Subject(s): PHARMACEUTICSOnline resources: Click here
In:
Indian journal of pharmaceutical sciencesSummary: Organic solvents are commonly used in in vitro drug metabolism studies as co-solvents for lipophilic substrate/
new chemical entities. The effects of 1 % v/v final concentration of individual, binary and ternary mixtures of
methanol, acetonitrile and dimethyl sulfoxide on human plasma esterases were investigated. The hydrolysis
of p-nitrophenyl acetate to p-nitrophenol was monitored by ultraviolet spectrophotometry to follow
esterase activity. Results indicated that the mixtures always showed less inhibition of esterase as compared
to theoretically calculated additive inhibition based on individual solvent data. Results also indicated that
dimethyl sulfoxide was the most-inhibitory solvent (59-64 % inhibition at 1 % v/v final concentration in
incubation) and mixtures containing the least concentration of dimethyl sulfoxide caused the least inhibition
of human plasma esterases.
| Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
|---|---|---|---|---|---|---|
Articles Abstract Database
|
School of Pharmacy Archieval Section | Not for loan | 2024-0427 |
Organic solvents are commonly used in in vitro drug metabolism studies as co-solvents for lipophilic substrate/
new chemical entities. The effects of 1 % v/v final concentration of individual, binary and ternary mixtures of
methanol, acetonitrile and dimethyl sulfoxide on human plasma esterases were investigated. The hydrolysis
of p-nitrophenyl acetate to p-nitrophenol was monitored by ultraviolet spectrophotometry to follow
esterase activity. Results indicated that the mixtures always showed less inhibition of esterase as compared
to theoretically calculated additive inhibition based on individual solvent data. Results also indicated that
dimethyl sulfoxide was the most-inhibitory solvent (59-64 % inhibition at 1 % v/v final concentration in
incubation) and mixtures containing the least concentration of dimethyl sulfoxide caused the least inhibition
of human plasma esterases.
Click on an image to view it in the image viewer
There are no comments for this item.